Hollow microspheres of diclofenac sodium - a gastroretentive controlled delivery system.
Most of the floating systems have an inherent drawback of high variability in the GI transit time, invariably affecting the bioavailability of drug. To overcome it, a multiple unit floating system with extended GI transit time, capable of distributing widely throughout the GIT for effective enteric release of the drug has been sought. Microballoons loaded with drug in their outer polymer shells were prepared by novel emulsion solvent diffusion method. The ethanol: dicloromethane solution of drug and Eudragit-S were poured into an aqueous solution of PVA that was thermally controlled at 40 degrees C. The gas phase generated in the dispersed polymer droplet by the evaporation of solvent formed an internal cavity in the microsphere of the polymer with the drug. The flowability of the resulting microballoons improved when compared to pure drug. The microballoons on floatation along with the surfactant, floated continuously for more than 12 hours in the acidic medium in-vitro conditions. The in-vitro drug release profile of the formulation in the simulated gastric buffer showed no drug release, which emphasizes the enteric release property and in simulated intestinal buffer, a slow and controlled drug release of 60 to 84% was obtained over a period of 8 hours. Drug release was significantly affected by increased drug to polymer concentration at pH 6.8. The formulation was found to be physically and chemically stable as per the ICH guidelines.
Bv
Basavaraj
B
Department of Pharmaceutics, MS Ramaiah College of Pharmacy, MSR Nagar, MSRIT Post, Bangalore-560 054, India. bvbasu@rediffmail.com
R
Deveswaran
D
S
Bharath
B
Abraham
Sindhu
S
Furtado
Sharon
S
V
Madhavan
M
D000284:Administration, Oral; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004008:Diclofenac / Q000008:administration & dosage / Q000737:chemistry*; D004355:Drug Stability; D000431:Ethanol / Q000737:chemistry; D005750:Gastric Juice / Q000737:chemistry; D005772:Gastrointestinal Transit; D006863:Hydrogen-Ion Concentration; D007419:Intestinal Secretions / Q000737:chemistry; D008863:Microspheres; D011109:Polymethacrylic Acids / Q000737:chemistry; D011142:Polyvinyl Alcohol / Q000737:chemistry; D016062:Porosity; D012995:Solubility; D013678:Technology, Pharmaceutical / Q000379:methods; D013997:Time Factors
D003692:Delayed-Action Preparations; D011109:Polymethacrylic Acids; D004008:Diclofenac; C038300:methylmethacrylate-methacrylic acid copolymer; D000431:Ethanol; D011142:Polyvinyl Alcohol